Fiboflapon sodium

Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood[1].

Product Specifications

CAS Number

[1196070-26-4]

Product Name Alternative

GSK2190915 (sodium salt) ; AM-803 sodium

UNSPSC

12352005

Target

FLAP; Leukotriene Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/GSK2190915-sodium-salt.html

Concentration

10mM

Purity

99.46

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC(C(O[Na])=O)(C)CC1=C(SC(C)(C)C)C2=CC(OCC3=CC=C(C)C=N3)=CC=C2N1CC4=CC=C(C5=CN=C(OCC)C=C5)C=C4

Molecular Formula

C38H42N3NaO4S

Molecular Weight

659.81

References & Citations

[1]Stock NS, et al. 5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4- (6-ethoxypyridin-3-yl) benzyl]-5- (5-methylpyridin-2-ylmethoxy) -1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor. J Med Chem. 2011 Dec 8;54 (23) :8013-29.|[2]Lorrain DS, et al. Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation. Eur J Pharmacol. 2010 Aug 25;640 (1-3) :211-8.